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Product name : Bilastine
Item : CR1868
Price : 200mg, $459;500mg, $850; 1g, $1195; 2g, $1795
contact : Send inquiry to: info@acesobio.com
CAS : 202189-78-4
Molecular Weight : 463.61
Formula : C₂₈H₃₇N₃O₃
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order
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Details:
 Chemical Information
M.Wt 463.61 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C28H37N3O3
CAS No 202189-78-4
Solubility

DMSO



Biological Activity of Bilastine

 

Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria.
Target: Histamine H1 Receptor
Bilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guinea-pig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening conducted to determine the binding capacity of bilastine to 30 different receptors [1]. Bilastine distribution has an apparent volume of distribution of 1.29 L/kg, and has an elimination half-life of 14.5 h and plasma protein binding of 84-90% [2].
 

 

[1]. Corcostegui, R., et al., Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity. Drugs R D, 2005. 6(6): p. 371-84.

[2]. Jauregizar, N., et al., Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine. Clin Pharmacokinet, 2009. 48(8): p. 543-54.


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